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WO2000032160A1 - Procedes pour reduire l'astringence des composes stanneux de compositions de dentifrice - Google Patents

Procedes pour reduire l'astringence des composes stanneux de compositions de dentifrice Download PDF

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Publication number
WO2000032160A1
WO2000032160A1 PCT/US1999/027810 US9927810W WO0032160A1 WO 2000032160 A1 WO2000032160 A1 WO 2000032160A1 US 9927810 W US9927810 W US 9927810W WO 0032160 A1 WO0032160 A1 WO 0032160A1
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WO
WIPO (PCT)
Prior art keywords
stannous
dentifrice composition
dentifrice
polyphosphate
poloxamer
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
Application number
PCT/US1999/027810
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English (en)
Inventor
William Michael Glandorf
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Procter and Gamble Co
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Procter and Gamble Co
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority to AU20288/00A priority Critical patent/AU757450B2/en
Priority to BR9915753-5A priority patent/BR9915753A/pt
Priority to KR1020017006720A priority patent/KR20010092452A/ko
Priority to EP99963959A priority patent/EP1135098B1/fr
Priority to HU0104746A priority patent/HUP0104746A3/hu
Priority to CA002348237A priority patent/CA2348237C/fr
Application filed by Procter and Gamble Co filed Critical Procter and Gamble Co
Priority to DE69928562T priority patent/DE69928562T2/de
Priority to JP2000584857A priority patent/JP2002531388A/ja
Priority to AT99963959T priority patent/ATE310493T1/de
Publication of WO2000032160A1 publication Critical patent/WO2000032160A1/fr
Anticipated expiration legal-status Critical
Priority to NO20012661A priority patent/NO20012661D0/no
Ceased legal-status Critical Current

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
    • A61K8/24—Phosphorous; Compounds thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
    • A61K8/20—Halogens; Compounds thereof
    • A61K8/21—Fluorides; Derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
    • A61K8/90—Block copolymers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q11/00—Preparations for care of the teeth, of the oral cavity or of dentures; Dentifrices, e.g. toothpastes; Mouth rinses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/40—Chemical, physico-chemical or functional or structural properties of particular ingredients
    • A61K2800/52—Stabilizers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/80—Process related aspects concerning the preparation of the cosmetic composition or the storage or application thereof
    • A61K2800/88—Two- or multipart kits

Definitions

  • the present invention relates to a method of reducing the astringency of dentifrice composition containing stannous.
  • the present inventor has discovered that the use of a poloxamer will reduce the astringency, bitterness, and sourness that is associated with stannous. It has also been discovered that certain polyphosphates, in particular, linear
  • polyphosphates with average chain lengths of about 4 or more will also help to reduce the astringency of the stannous. This reduction in astringency occurs without reducing the efficacy of the stannous from either the poloxamer or the polyphosphate.
  • stannous as used herein, is defined to mean the stannous that is in a dentifrice. It may refer to the stannous ions that are provided by a stannous salt. Stannous 0 salts which contain stannous ions are commonly known. Stannous has been found to provide antigingivitis and antiplaque benefits. In addition, stannous may also help to improve breath and reduce sensitivity. Dentifrices containing stannous are also known to cause staining on a subject's tooth surface as well as having an astringent feel. The astringency is most noticeable after use of the product. U.S.
  • patent 5,780,015 describes 5 the use of an oxyethylated reaction product of hydrogenated castor oil to help reduce astringency. To improve consumer acceptance of dentifrice composition containing stannous, additional dentifrice compositions containing the benefits of stannous but without the astringency are needed.
  • the dentifrice composition comprises stannous ions, poloxamer, and aqueous carriers.
  • the efficacy of this dentifrice composition containing stannous will not be reduced by the poloxamer.
  • the dentifrice composition may also contain a polyphosphate as long as the dentifrice has a low water content and does not contain stannous fluoride as the source of stannous ions. The polyphosphate will also not reduce the efficacy of the stannous.
  • the dentifrice composition may be a dual phase composition.
  • the first dentifrice composition will contain a polyphosphate having an average chain length of about 4 or more and have a low water content and the second dentifrice composition will contain stannous ions.
  • the poloxamer will be present in the first or second dentifrice compositions or both compositions.
  • the present invention relates to methods for reducing the astringency of dentifrice composition containing stannous comprising administering to the subject a dentifrice composition comprising stannous.
  • the dentifrice composition comprises stannous ions, poloxamer, and aqueous carriers.
  • the efficacy of this dentifrice composition containing stannous will not be reduced by the poloxamer.
  • the dentifrice composition may also contain a polyphosphate as long as the water content is limited and the stannous ion is not provided from stannous fluoride. The polyphosphate will also not reduce the efficacy of the stannous.
  • the dentifrice composition may be a dual phase composition.
  • the first dentifrice composition will contain a polyphosphate having an average chain length of about 4 or more and have a limited water content while the second dentifrice composition will contain stannous ions.
  • the poloxamer will be present in the first or second dentifrice compositions or both compositions. Neither the polyphosphate or the poloxamer will reduce the efficacy of the stannous.
  • the oral formulation of the present invention may be in the form of a toothpaste or dentifrice.
  • dentifrice means paste, gel, or liquid formulations unless otherwise specified.
  • the dentifrice composition may be in any desired form, such as deep striped, surface striped, mulitlayered, having the gel surrounding the paste, or any combination thereof.
  • Each dentifrice composition may be a single phase dentifrice or may be part of a dual phase dentifrice and contained in a physically separated compartment of a dispenser and dispensed side-by-side.
  • dispenser means any pump, tube, or container suitable for dispensing toothpaste.
  • the dentifrice composition is a product, which in the ordinary course of administration, is not intentionally swallowed for purposes of systemic administration of particular therapeutic agents, but is rather retained in the oral cavity of a subject for a time sufficient to contact substantially all of the tooth surfaces and/or oral tissues for purposes of oral activity.
  • aqueous carrier as used herein means any safe and effective materials for use in the compositions of the present invention.
  • Such materials include fluoride ion sources, anticalculus agents, antibacterial agents, abrasive polishing materials, peroxide sources, alkali metal bicarbonate salts, thickening materials, humectants, water, surfactants, buffering agents, titanium dioxide, flavor system, sweetening agents, coloring agents, and mixtures thereof.
  • reducing the astringency of dentifrice compositions containing stannous means that the level of astringency noticed by subjects is statistically significantly reduced from a control.
  • Not reducing the efficacy of the stannous means where the efficacy of the stannous is not statistically significantly reduced from a control.
  • a control product containing stannous may be Crest Gum Care.
  • the present compositions comprise essential components, as well as optional components.
  • the essential and optional components of the compositions of the present invention are described in the following paragraphs.
  • Stannous Ions The present invention includes a stannous ion.
  • the stannous ion generally comes from a stannous salt that is added to a dentifrice.
  • Stannous has been found to help in the reduction gingivitis, plaque, sensitivity, and improved breath benefits.
  • the stannous in a dentifrice composition will provide efficacy to a subject using the dentifrice. "Efficacy" is defined as a noticeable amount of reduction in gingivitis as measured by the Plaque Glycolysis Regrowth Model (PGRM).
  • PGRM Plaque Glycolysis Regrowth Model
  • the present inventors have found a way to reducing the astringency caused by the stannous while preventing the efficacy of the stannous from being reduced. Specifically, the efficacy of the stannous is not reduced by the poloxamer or polyphosphate even though they will each reduce the astringency of the stannous. Therefore, the efficacy of the stannous is maintained at a level found in dentifrices containing stannous which are known for reducing gingivitis, such as Crest Gum Care. It has also been found that the polyphosphate having an average chain length of about 4 or more will also help to reduce the staining caused by the stannous.
  • Stannous ions are found in the dentifrice composition in an effective amount.
  • An effective amount is defined as from about 3,000 ppm to about 15,000 ppm. Below 3,000 ppm stannous the efficacy of the stannous is not significant.
  • the stannous anion is present in an amount of about 5,000 ppm to about 13,000 ppm and more preferably from about 7,000 ppm to about 10,000 ppm. This is the total amount of stannous ion that is delivered to the oral cavity.
  • Dentifrices containing stannous salts, particularly stannous fluoride and stannous chloride are described in U.S. Patent 5,004,597 to Majeti et al, incorporated herein in its entirety.
  • stannous salt dentifrices are found in U.S. Patent 5,578,293 and 5,578,293.
  • the preferred stannous salts are stannous fluoride and stannous chloride dihydrate.
  • Other stannous salts include stannous acetate.
  • the combined stannous salts will be present in an amount of from about 0.25%o to about 11%, by weight of the final composition.
  • the stannous salts are present in an amount of from about 0.5 to about 7%, more preferably from about 1% to about 5%, and most preferably from about 1.5% to about 4%.
  • Poloxamer Poloxamer is classified as a nonionic surfactant.
  • Poloxamers are difunctional block-polymers terminating in primary hydroxyl groups with molecular weights ranging from 1,000 to above 15,000. Poloxamers are sold under the tradename of Pluronics by BASF.
  • the most preferred poloxamer for this invention is poloxamer 407. To have a measurable impact on the astringency of the stannous, the poloxamer must be present in an amount of about 5% or more. The reduction of astringency is measured by taste, aftertaste, and astringency comments provided by subjects who brush with the dentifrice composition.
  • the poloxamer is present in an amount of from about 5% to about 50%, preferably from about 6%> to about 30%, more preferably from about 7% to about 20%o, and most preferably from about 8% to about 18%, by weight of the composition.
  • compositions with poloxamer levels of from about 10% or more and about 15% or more may be used. If a dual phase dentifrice is used, the total amount of poloxamer may be from all of the poloxamer being in one phase or from the poloxamer being divided into two phases.
  • the present invention may also include a polyphosphate source.
  • Polyphosphates are known to help retard calculus formation.
  • the present inventor has also found that a polyphosphates having an average chain length of about 4 or more will also help to reduce the astringency of a stannous salt.
  • the polyphosphate must be in a composition with a lower water content to prevent the polyphosphate from hydrolyzing. The reduction in astringency will occur if the stannous salt and polyphosphate are in the same phase or are in separate phases and only interact once dispensed on a toothbrush.
  • the poloxamer may also be in the same phase as the polyphosphate or the stannous salt, or all three ingredients may be in the same phase. If stannous fluoride is the stannous salt, the fluoride will react with the polyphosphate. This reaction will cause monofluorophosphate to be formed which inhibits the efficacy of the fluoride and an inhibition of the anti-tartar efficacy of the polyphosphate also results. Therefore, to provide an efficacious formula, the polyphosphate and stannous fluoride should be in separate phases. If the stannous salt is not stannous fluoride, the stannous salt and polyphosphate may be in the same phase. It is unexpected that a polyphosphate having an average chain length of about 4 or more would provide this beneficial effect.
  • pyrophosphates will react with a stannous salt and form a sparingly soluble salt. This will inhibit the efficacy of the stannous salt and likely the anti-tartar efficacy of the 5 pyrophosphate. Therefore, it is unexpected that a polyphosphate with a longer chain length has a beneficial effect of reducing the astringency with the stannous salt.
  • a polyphosphate is generally understood to consist of two or more phosphate molecules arranged primarily in a linear configuration, although some cyclic derivatives may be present.
  • pyrophosphates are a polyphosphate
  • the polyphosphates i o desired are those having around four or more phosphate molecules.
  • the pyrophosphates are discussed separately.
  • the inorganic polyphosphate salts desired include tetrapolyphosphate and hexametaphosphate, among others. Polyphosphates larger than tetrapolyphosphate usually occur as amorphous glassy materials.
  • Preferred in this invention are the linear "glassy" polyphosphates having the formula:
  • XO(XPO ) n X wherein X is sodium or potassium and n averages from about 6 to about 125.
  • the polyphosphate source will typically comprise from about 1%) to about 20%, preferably from about 3% to about 17%, more preferably from 5 about 4% to about 15%, and most preferably from about 5% to about 13%, by weight of the dentifrice composition.
  • the ratio of total moles of polyphosphate anion to total moles of stannous ion should also be controlled. This ratio is from about 0.2: 1 to about 5: 1 , 0 preferably from about 0.5: 1 to about 3: 1, more preferably from about 0.6: 1 to about 2: 1 and most preferably from about 0.7: 1 to about 1.5: 1.
  • aqueous carriers typically comprise from about 40% to about 99%>, preferably from about 60% to about 98%, more preferably from about 15% to about 97%), and most preferably from about 90%> to about 95%, by weight of the dentifrice composition.
  • Total Water Content Water employed in the preparation of commercially suitable oral compositions should preferably be of low ion content and free of organic impurities.
  • water will generally comprise from about 5%o to about 70%, and preferably from about 10%o to about 50%, by weight of the composition herein. This water content may be in a single phase dentifrice or may be the resulting total water content of a dual phase dentifrice. If the dentifrice composition comprises the polyphosphate having an average chain length of about 4 or more, the dentifrice composition will comprise a lower level of water, generally from about 0% water up to about 20% total water. Preferably, the total water content is from about 2% to about 20%o, more preferably from about 4% to about 15%), and most preferably from about 5% to about 12%, by weight of the dentifrice composition.
  • the amounts of water include the free water which is added plus that which is introduced with other materials, such as with sorbitol, silica, surfactant solutions, and/or color solutions.
  • the dentifrice compositions of the present invention may incorporate a soluble fluoride source capable of providing free fluoride ions.
  • Soluble fluoride ion sources include sodium fluoride, stannous fluoride, indium fluoride, and sodium monofluorophosphate.
  • Stannous fluoride is the most preferred soluble fluoride ion source. This ingredient may serve as both the stannous ion and fluoride ion source. If a polyphosphate having a chain length of about 4 or more is in the same phase as the fluoride ion source, the preferred fluoride ion source is sodium monofluorophosphate.
  • compositions may contain a soluble fluoride ion source capable of providing from about 50 ppm to about 3500 ppm, and preferably from about 500 ppm to about 3000 ppm of free fluoride ions.
  • stannous fluoride may be present in the total dentifrice composition at an amount of from about 0.1%) to about 5%, preferably from about 0.2%o to about 1%, and more preferably from about 0.3 to about 0.6%, by weight of the total dentifrice composition.
  • the present compositions may contain a buffering agent.
  • Buffering agents refer to agents that can be used to adjust the pH of the compositions to a range of about pH 3.0 to about pH 10.
  • the phase of the dentifrice containing stannous will typically have a slurry pH of from about 3.0 to about 5.5, preferably from about 3.25 to about 5, and more preferably from about 3.4 to about 4.5.
  • the phase of the dentifrice containing the polyphosphate will typically have a slurry pH of from about 4.0 to about 10, preferably from about 4.5 to about 8, and more preferably from about 5.0 to about 7.0.
  • a dentifrice containing both stannous and polyphosphate in a single phase will typically have a pH of from about 4 to about 7, preferably from about 4.5 to about 6, and more preferably from about 5 to about 5.5.
  • the buffering agents include alkali metal hydroxides, carbonates, sesquicarbonates, borates, silicates, phosphates, imidazole, and mixtures thereof.
  • Specific buffering agents include monosodium phosphate, trisodium phosphate, sodium benzoate, benzoic acid, sodium hydroxide, potassium hydroxide, alkali metal carbonate salts, sodium carbonate, imidazole, pyrophosphate salts, citric acid, and sodium citrate.
  • Buffering agents are used at a level of from about 0.1% to about 30%, preferably from about 1%) to about 10%, and more preferably from about 1.5% to about 3%, by weight of the present composition.
  • Anticalculus agents include such materials known to be effective in reducing calcium phosphate mineral deposition related to calculus formation.
  • Agents included are pyrophosphates, tripolyphosphates, synthetic anionic polymers [including polyacrylates and copolymers of maleic anhydride or acid and methyl vinyl ether (e.g., Gantrez), as described, for example, in U.S.
  • Patent 4,627,977 to Gaffar et al., the disclosure of which is incorporated herein by reference in its entirety; as well as, e.g., polyamino propane sulfonic acid (AMPS)], zinc citrate trihydrate, diphosphonates (e.g., EHDP; AHP), polypeptides (such as polyaspartic and polyglutamic acids), and mixtures thereof.
  • AMPS polyamino propane sulfonic acid
  • An abrasive polishing material may also be included in the toothpaste compositions.
  • the abrasive polishing material contemplated for use in the compositions of the present invention can be any material which does not excessively abrade dentin.
  • Typical abrasive polishing materials include silicas including gels and precipitates; aluminas; phosphates including orthophosphates, polymetaphosphates, and pyrophosphates; and mixtures thereof.
  • abrasive materials such as particulate condensation products of urea and formaldehyde, and others such as disclosed by Cooley et al in U.S. Patent 3,070,510, issued Dec. 25, 1962, incorporated herein by reference. Mixtures of abrasives may also be used. If the dentifrice composition or particular phase comprises a polyphosphate having an average chain length of about 4 or more, calcium containing abrasives and alumina are not preferred abrasives. The most preferred abrasive is silica.
  • Silica dental abrasives of various types are preferred because of their unique benefits of exceptional dental cleaning and polishing performance without unduly abrading tooth enamel or dentine.
  • the silica abrasive polishing materials herein, as well as other abrasives generally have an average particle size ranging between about 0.1 to about 30 microns, and preferably from about 5 to about 15 microns.
  • the abrasive can be precipitated silica or silica gels such as the silica xerogels described in Pader et al., U.S. Patent 3,538,230, issued Mar. 2, 1970, and DiGiulio, U.S. Patent 3,862,307, issued Jan. 21 , 1975, both incorporated herein by reference.
  • silica xerogels marketed under the trade name "Syloid” by the W.R. Grace & Company, Davison Chemical Division.
  • precipitated silica materials such as those marketed by the J. M. Huber Corporation under the trade name, "Zeodent", particularly the silica carrying the designation "Zeodent 1 19".
  • the types of silica dental abrasives useful in the toothpastes of the present invention are described in more detail in Wason, U.S. Patent 4,340,583, issued July 29, 1982, incorporated herein by reference. Silica abrasives described in Rice, U.S.
  • the abrasive in the toothpaste compositions described herein is generally present at a level of from about 6% to about 70%) by weight of the composition.
  • toothpastes contain from about 10%o to about 50%) of abrasive, by weight of the dentifrice composition.
  • Peroxide Source may include a peroxide source in the dentifrice composition.
  • the peroxide source is selected from the group consisting of hydrogen peroxide, calcium peroxide, urea peroxide, and mixtures thereof.
  • the preferred peroxide source is calcium peroxide.
  • the following amounts represent the amount of peroxide raw material, although the peroxide source may contain ingredients other than the peroxide raw material.
  • the present composition may contain from about 0.01 % to about 10%, preferably from about 0.1%) to about 5%, more preferably from about 0.2% to about 3%, and most preferably from about 0.3% to about 0.8% of a peroxide source, by weight of the dentifrice composition.
  • Alkali Metal Bicarbonate Salt may also include an alkali metal bicarbonate salt. Alkali metal bicarbonate salts are soluble in water and unless stabilized, tend to release carbon dioxide in an aqueous system. Sodium bicarbonate, also known as baking soda, is the preferred alkali metal bicarbonate salt.
  • the alkali metal bicarbonate salt also functions as a buffering agent.
  • the present composition may contain from about 0.5% to about 50%, preferably from about 0.5% to about 30%, more preferably from about 2% to about 20%), and most preferably from about 5% to about 18% of an alkali metal bicarbonate salt, by weight of the dentifrice composition. Additional Aqueous Carriers
  • compositions in the form of toothpastes typically contain some thickening material or binders to provide a desirable consistency.
  • Preferred thickening agents are carboxyvinyl polymers, carrageenan, hydroxyethyl cellulose, and water soluble salts of cellulose ethers such as sodium carboxymethylcellulose and sodium hydroxyethyl cellulose.
  • Natural gums such as gum karaya, xanthan gum, gum arabic, and gum tragacanth can also be used.
  • Colloidal magnesium aluminum silicate or finely divided silica can be used as part of the thickening agent to further improve texture.
  • Thickening agents can be used in an of amount from about 0.1 % to about 15%, by weight of the dentifrice composition.
  • humectant serves to keep toothpaste compositions from hardening upon exposure to air and certain humectants can also impart desirable sweetness of flavor to toothpaste compositions.
  • Suitable humectants for use in the invention include glycerin, sorbitol, polyethylene glycol, propylene glycol, xylitol, and other edible polyhydric alcohols.
  • the humectant generally comprises from about 0% to 70%, and preferably from about 15% to 55%>, by weight of the composition.
  • the present compositions may also comprise surfactants, also commonly referred to as sudsing agents.
  • Surfactants in addition to the nonionic surfactant poloxamer, may also be incorporated into the present dentifrice composition. Suitable surfactants are those which are reasonably stable and foam throughout a wide pH range.
  • the surfactant may be anionic, nonionic, amphoteric, zwitterionic, cationic, or mixtures thereof.
  • Anionic surfactants useful herein include the water-soluble salts of alkyl sulfates having from 8 to 20 carbon atoms in the alkyl radical (e.g., sodium alkyl sulfate) and the water- soluble salts of sulfonated monoglycerides of fatty acids having from 8 to 20 carbon atoms.
  • anionic surfactants of this type.
  • Other suitable anionic surfactants are sarcosinates, such as sodium lauroyl sarcosinate, taurates, sodium lauryl sulfoacetate, sodium lauroyl isethionate, sodium laureth carboxylate, and sodium dodecyl benzenesulfonate. Mixtures of anionic surfactants can also be employed.
  • Many suitable anionic surfactants are disclosed by Agricola et al, U.S. Patent 3,959,458, issued May 25, 1976, incorporated herein in its entirety by reference.
  • Nonionic surfactants which can be used in the compositions of the present invention can be broadly defined as compounds produced by the condensation of alkylene oxide groups (hydrophilic in nature) with an organic hydrophobic compound which may be aliphatic or alkyl-aromatic in nature.
  • nonionic surfactants include polyoxyethylene, polyoxyethylene sorbitan esters (sold under trade name Tweens), Polyoxyl 40 hydrogenated caster oil, fatty alcohol ethoxylates, polyethylene oxide condensates of alkyl phenols, products derived from the condensation of ethylene oxide with the reaction product of propylene oxide and ethylene diamine, ethylene oxide condensates of aliphatic alcohols, long chain tertiary amine oxides, long chain tertiary phosphine oxides, long chain dialkyl sulfoxides, and mixtures of such materials.
  • suitable nonionic surfactants include polyoxyethylene, polyoxyethylene sorbitan esters (sold under trade name Tweens), Polyoxyl 40 hydrogenated caster oil, fatty alcohol ethoxylates, polyethylene oxide condensates of alkyl phenols, products derived from the condensation of ethylene oxide with the reaction product of propylene oxide and ethylene diamine, ethylene oxide condensates of
  • amphoteric surfactants useful in the present invention can be broadly described as derivatives of aliphatic secondary and tertiary amines in which the aliphatic radical can be a straight chain or branched and wherein one of the aliphatic substituents contains from about 8 to about 18 carbon atoms and one contains an anionic water-solubilizing group, e.g., carboxylate, sulfonate, sulfate, phosphate, or phosphonate.
  • suitable amphoteric surfactants are betaines, specifically cocamidopropyl betaine. Mixtures of amphoteric surfactants can also be employed.
  • the present composition typically comprises one or more surfactants each at a level of from about 0.25%) to about 12%>, preferably from about 0.5%> to about 8%, and most preferably from about 1%) to about 6%>, by weight of the composition.
  • Titanium dioxide may also be added to the present composition. Titanium dioxide is a white powder which adds opacity to the compositions. Titanium dioxide generally comprises from about 0.25% to about 5%>, by weight of the composition.
  • Coloring agents may also be added to the present composition.
  • the coloring agent may be in the form of an aqueous solution, preferably 1%> coloring agent in a solution of water.
  • Color solutions generally comprise from about 0.01 % to about 5%>, by weight of the composition.
  • a flavor system can also be added to the compositions.
  • Suitable flavoring components include oil of wintergreen, oil of peppermint, oil of spearmint, clove bud oil, menthol, anethole, methyl salicylate, eucalyptol, cassia, 1-menthyl acetate, sage, eugenol, parsley oil, oxanone, alpha-irisone, marjoram, lemon, orange, propenyl guaethol, cinnamon, vanillin, ethyl vanillin, heliotropine, 4-cis-heptenal, diacetyl, methyl-para-tert- butyl phenyl acetate, and mixtures thereof. Coolants may also be part of the flavor system.
  • Preferred coolants in the present compositions are the paramenthan carboxyamide agents such as N-ethyl-p-menthan-3-carboxamide (known commercially as "WS-3") and mixtures thereof.
  • a flavor system is generally used in the compositions at levels of from about 0.001% to about 5%, by weight of the composition.
  • Sweetening agents can be added to the compositions. These include saccharin, dextrose, sucrose, lactose, maltose, xylitol, levulose, aspartame, sodium cyclamate, D- tryptophan, dihydrochalcones, acesulfame, and mixtures thereof.
  • Various coloring agents may also be incorporated in the present invention. Sweetening agents and coloring agents are generally used in toothpastes at levels of from about 0.005%> to about 5%, by weight of the composition.
  • the present invention may also include other agents, such as antimicrobial agents.
  • antimicrobial agents include water insoluble non-cationic antimicrobial agents such as halogenated diphenyl ethers, phenolic compounds including phenol and its homologs, mono and poly-alkyl and aromatic halophenols, resorcinol and its derivatives, bisphenohc compounds and halogenated salicylanilides, benzoic esters, and halogenated carbanilides.
  • the water soluble antimicrobials include quaternary ammonium salts and bis-biquanide salts, among others. Triclosan monophosphate is an additional water soluble antimicrobial agent.
  • the quaternary ammonium agents include those in which one or two of the substitutes on the quaternary nitrogen has a carbon chain length (typically alkyl group) from about 8 to about 20, typically from about 10 to about 18 carbon atoms while the remaining substitutes (typically alkyl or benzyl group) have a lower number of carbon atoms, such as from about 1 to about 7 carbon atoms, typically methyl or ethyl groups.
  • Specific antimicrobial agents include chlorhexidine, triclosan, triclosan monophosphate, and flavor oils such as thymol. Triclosan and other agents of this type are disclosed in Parran, Jr. et al, U.S. Patent 5,015,466, issued May 14, 1991, and U.S. Patent 4,894,220, Jan. 16, 1990 to Nabi et al., incorporated herein by reference.
  • the water insoluble antimicrobial agents, water soluble agents, and ezymes may be present in either the first or second dentifrice compsoitions.
  • the quaternary ammonium agents, stannous salts, and substituted guanidines are preferably present in the second dentifrice composition. These agents may be present at levels of from about 0.01% to about 1.5%), by weight of the dentifrice composition.
  • the dentifrice compositions may be a paste, gel, or any configuration or combination thereof. If a dual phase dentifrice composition is desired, the first and second dentifrice compositions will be physically separated in a dentifrice dispenser. It is then preferred that one of the dentifrice composition be a paste and the other dentifrice composition be a gel.
  • the dispenser may be a tube, pump, or any other container suitable for dispensing toothpaste. Dual compartment packages suitable for this purpose are described in U.S. Patent 4,528,180, issued July 9, 1985; U.S. Patent 4,687,663, issued August 18, 1987; and 4,849,213, issued July 18, 1989, all to Shaeffer, all incorporated herein in their entirety.
  • the dispenser will deliver approximately equal amounts of each dentifrice composition through an opening.
  • the compositions may intermix once dispensed.
  • the oral formulation may be delivered from a kit containing two separate dispensers which are used to deliver two dentifrice compositions that are both used simultaneously.
  • the present invention relates to a method of reducing the astringency of dentifrice compositions containing stannous.
  • a dentifrice composition containing stannous typically has a strong astringent taste. Each subject using the dentifrice may notice a different degree of astringency.
  • the present invention is a method to reduce the level of astringency that is noticed by a subject using a dentifrice composition containing stannous. This method may not eliminate the astringency completely, but it will significantly reduce the level of astringency.
  • the method of reducing the astringency of dentifrice compositions containing stannous comprises administering to the subject a dentifrice composition comprising stannous.
  • the method may include preparing a dentifrice composition containing stannous and having a subject use the dentifrice composition comprising the stannous.
  • the term "administer" is defined as using the dentifrice by any retention of the dentifrice composition in the oral cavity for a time sufficient to contact substantially all of the dental surfaces and/or oral tissues for pu ⁇ oses of oral activity.
  • the administration is from brushing with the dentifrice or from rinsing with a dentifoce slurry.
  • a subject is defined as any person or animal who uses the dentifoce composition. Examples & Method of Manufacturing
  • the first dentifrice composition is made as follows: Add the water, sorbitol, and saccharin to a mixing vessel and heat to at least 50°C. Add the sodium gluconate and mix until completely dissolved. Add stannous fluoride and mix until completely dissolved. Add stannous chloride and mix until completely dissolved. Add sodium hydroxide and mix until neutralization is complete. Disperse carboxymethyl cellulose and hydroxyethyl cellulose in glycerin. Add this glycerin slurry to the mixing vessel and mix well. Next add silica. Mix well. Cool the mixing vessel to less than 30°C and add the flavor and sodium lauryl sulphate. Mix until homogeneous.
  • the second dentifrice composition is made as follows: Add water, glycerin, saccharin and xylitol to the main mix vessel and heat to at least 60°C. Add poloxamer, color and flavor and mix until poloxamer dissolves. Cool batch to less than 30°C.
  • Poloxamer 407 3.000 Sodium Saccharin 0.300
  • Examples II, III, IV, and V are prepared as follows.
  • the first dentifrice compositions are prepared by adding the water, sodium benzoate and saccharin to a mixing vessel. Disperse carboxymethyl cellulose, xanthan gum and polyoxyethylene (if used) in glycerin. Add this glycerin slurry to the mixing vessel, mixing well and heating to at least 40°C. Dissolve the benzoic acid in a mixture of flavor, propylene glycol, poloxamer (if used), sodium lauryl sulphate and polyethylene glycol, then add to the mixing vessel. Next add titanium dioxide and silica. Mix well. Cool the mixing vessel to less than 30°C and add the polyphosphate. Mix until homogeneous.
  • the second dentifrice compositions are prepared as follows. Add water, color, and glycerin to the main mix vessel and heat to at least 50°C. Add the sodium gluconate and mix until completely dissolved. Add stannous fluoride and mix until completely dissolved. Add stannous chloride and mix until completely dissolved. Add sodium hydroxide, saccharin and silica and mix well. Add poloxamer and flavor and mix until poloxamer dissolves. Cool batch to less than 30°C.
  • Example VI is prepared as follows: Add the water, color, glycerin and saccharin to a mixing vessel. And heat to at least 50°C. Add the sodium gluconate and mix until completely dissolved. Add stannous fluoride and mix until completely dissolved. Add stannous chloride and mix until completely dissolved. Add sodium hydroxide and mix until the neutralization is complete. Next add silica and mix well. Add the poloxamer and flavor and mix until the poloxamer dissolves. Cool the mixing vessel to less than 30°C and add the sodium lauryl sulphate. Mix until homogeneous.
  • Example VJJ is prepared as follows: Add the water, sorbitol and saccharin to a mixing vessel. And heat to at least 50°C. Add the sodium gluconate and mix until completely dissolved. Add stannous fluoride and mix until completely dissolved. Add stannous chloride and mix until completely dissolved. Add sodium hydroxide and mix until the neutralization is complete. Disperse hydroxyethyl cellulose, xanthan gum and polyoxyethylene in glycerin and polyethylene glycol. Add this slurry to the mixing vessel, mixing well. Next add silica and titanium dioxide and mix well. Add the poloxamer and flavor and mix until the poloxamer dissolves. Cool the mixing vessel to less than 30°C and add the sodium lauryl sulphate. Mix until homogeneous.
  • Example Vi ⁇ is prepared as follows: Add the water, color, glycerin and saccharin to a mixing vessel. And heat to at least 50°C. Add the sodium gluconate and mix until completely dissolved. Add stannous fluoride and mix until completely dissolved. Add stannous chloride and mix until completely dissolved. Add sodium hydroxide and mix until the neutralization is complete. Add the poloxamer and flavor and mix until the poloxamer dissolves. Cool the mixing vessel to less than 30°C and add the sodium lauryl sulphate. Mix until homogeneous.

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Abstract

Cette invention se rapporte à des procédés servant à réduire l'astringence de compositions de dentifrice contenant des composés stanneux, ces procédés consistant à administrer à un sujet une telle composition de dentifrice contenant des composés stanneux. Une telle composition de dentifrice renferme des ions stanneux, un poloxamère et des supports aqueux. L'efficacité de cette composition de dentifrice contenant des composés stanneux n'est pas réduite par le poloxamère. Cette composition de dentifrice peut également contenir un polyphosphate, pour autant que la teneur en eau est limitée et que l'ion stanneux n'est pas fourni par du fluorure d'étain. Le polyphosphate ne va pas réduire l'efficacité du composé stanneux. Dans une variante, une telle composition de dentifrice peut également être constituée par une composition à deux phases. La première composition de dentifrice va contenir un polyphosphate ayant une longueur de chaîne moyenne d'environ 4 ou davantage et une teneur en eau limitée, alors que la seconde composition de dentifrice va contenir des ions stanneux. Dans une telle composition à deux phases, le poloxamère peut être présent dans la première ou dans la seconde composition de dentifrice ou dans les deux compositions. Ni le polyphosphate ni le poloxamère ne vont réduire l'efficacité du composé stanneux.
PCT/US1999/027810 1998-11-30 1999-11-23 Procedes pour reduire l'astringence des composes stanneux de compositions de dentifrice Ceased WO2000032160A1 (fr)

Priority Applications (10)

Application Number Priority Date Filing Date Title
DE69928562T DE69928562T2 (de) 1998-11-30 1999-11-23 Methoden zur reduktion der adstringierenden wirkung von zinn enthaltenden zahnpastazusammensetzungen
BR9915753-5A BR9915753A (pt) 1998-11-30 1999-11-23 Métodos para reduzir a adstringência de estanosos em composições de dentifrìcios
KR1020017006720A KR20010092452A (ko) 1998-11-30 1999-11-23 치약 조성물 중 주석의 수렴성 감소 방법
EP99963959A EP1135098B1 (fr) 1998-11-30 1999-11-23 Procedes pour reduire l'astringence des composes stanneux de compositions de dentifrice
HU0104746A HUP0104746A3 (en) 1998-11-30 1999-11-23 Methods of reducing the astringency of stannous in dentifrice compositions
AU20288/00A AU757450B2 (en) 1998-11-30 1999-11-23 Methods of reducing the astringency of stannous in dentifrice compositions
AT99963959T ATE310493T1 (de) 1998-11-30 1999-11-23 Methoden zur reduktion der adstringierenden wirkung von zinn enthaltenden zahnpastazusammensetzungen
CA002348237A CA2348237C (fr) 1998-11-30 1999-11-23 Procedes pour reduire l'astringence des composes stanneux de compositions de dentifrice
JP2000584857A JP2002531388A (ja) 1998-11-30 1999-11-23 歯みがき剤組成物中の第一すずの収斂性を低減する方法
NO20012661A NO20012661D0 (no) 1998-11-30 2001-05-30 Fremgangsmåte for å redusere astringens av tinn(II) i dentifriciumsammensetninger

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US09/203,215 US6187295B1 (en) 1996-11-21 1998-11-30 Methods of reducing the astringency of stannous in dentifrice compositions

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AT (1) ATE310493T1 (fr)
AU (1) AU757450B2 (fr)
BR (1) BR9915753A (fr)
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ES (1) ES2252992T3 (fr)
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WO1998051271A1 (fr) * 1997-05-14 1998-11-19 Colgate-Palmolive Company Dentifrice desensibilisateur a astringence limitee
WO1999020238A1 (fr) * 1997-10-23 1999-04-29 Warner-Lambert Company Produits oraux contenant un ion metallique a astringence reduite
WO1999053893A1 (fr) * 1998-04-23 1999-10-28 Colgate-Palmolive Company Dentifrice de desensibilisation contenant des sels de potassium et d'etain

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WO2001034108A1 (fr) 1999-11-12 2001-05-17 The Procter & Gamble Company Compositions buccales ameliorees contenant des sels d'etain
EP2238965A1 (fr) * 1999-11-12 2010-10-13 The Procter & Gamble Company Compositions orales contenant des ions d'etain
WO2001034109A1 (fr) * 1999-11-12 2001-05-17 The Procter & Gamble Company Compositions orales stanneuses a deux phases ameliorees
WO2001068046A3 (fr) * 2000-03-14 2002-02-21 Procter & Gamble Compositions de dentifrice stables comprenant du polyphosphate, du fluor et un composant stanneux
WO2002002128A3 (fr) * 2000-06-30 2002-04-25 Procter & Gamble Renforcement global de l'organisme
JP2008143910A (ja) * 2000-06-30 2008-06-26 Procter & Gamble Co 局所用口腔組成物
CN100360109C (zh) * 2001-05-15 2008-01-09 宝洁公司 口腔护理组合物
WO2008041055A1 (fr) * 2006-10-02 2008-04-10 The Procter & Gamble Company Compositions d'hygiène buccale stanneuses
RU2469700C2 (ru) * 2006-10-02 2012-12-20 Дзе Проктер Энд Гэмбл Компани Композиции для ухода за полостью рта, содержащие олово (ii)
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US10653605B2 (en) 2011-02-18 2020-05-19 Gaba International Holding Gmbh Dentifrice composition
WO2013095366A1 (fr) * 2011-12-20 2013-06-27 Colgate-Palmolive Company Compositions d'hygiène orale
US9522103B2 (en) 2011-12-20 2016-12-20 Colgate-Palmolive Company Oral care compositions
CN104023796B (zh) * 2011-12-20 2018-02-09 高露洁-棕榄公司 口腔护理组合物
CN104023796A (zh) * 2011-12-20 2014-09-03 高露洁-棕榄公司 口腔护理组合物
WO2015168879A1 (fr) * 2014-05-07 2015-11-12 The Procter & Gamble Company Compositions de soin bucco-dentaire
WO2015168877A1 (fr) * 2014-05-07 2015-11-12 The Procter & Gamble Company Compositions de soin bucco-dentaire
AU2014393337B2 (en) * 2014-05-07 2018-01-04 The Procter & Gamble Company Oral care compositions
WO2016025694A1 (fr) * 2014-08-15 2016-02-18 The Procter & Gamble Company Compositions pour l'hygiène bucco-dentaire améliorant les perceptions sensorielles
CN106659650A (zh) * 2014-08-15 2017-05-10 宝洁公司 感官体验增强的口腔护理组合物

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EP1135098B1 (fr) 2005-11-23
BR9915753A (pt) 2001-09-04
NO20012661L (no) 2001-05-30
US6187295B1 (en) 2001-02-13
AU2028800A (en) 2000-06-19
TR200101532T2 (tr) 2001-10-22
CA2348237A1 (fr) 2000-06-08
AU757450B2 (en) 2003-02-20
EP1135098A1 (fr) 2001-09-26
DE69928562T2 (de) 2006-08-03
HUP0104746A2 (hu) 2002-04-29
CA2348237C (fr) 2003-11-11
DE69928562D1 (de) 2005-12-29
ES2252992T3 (es) 2006-05-16
CN1328441A (zh) 2001-12-26
CN1154471C (zh) 2004-06-23
HUP0104746A3 (en) 2006-02-28
CZ20011526A3 (cs) 2001-10-17
JP2002531388A (ja) 2002-09-24
NO20012661D0 (no) 2001-05-30
ATE310493T1 (de) 2005-12-15
KR20010092452A (ko) 2001-10-25

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